Bioorganic & Medicinal Chemistry Letters 2006-06-15

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

Ting-Yueh Tsai, Mohane Selvaraj Coumar, Tsu Hsu, Hsing-Pang Hsieh, Chia-Hui Chien, Chiung-Tong Chen, Chung-Nien Chang, Yu-Kang Lo, Ssu-Hui Wu, Chung-Yu Huang, Yu-Wen Huang, Min-Hsien Wang, Hsin-Yi Wu, Hong-Jen Lee, Xin Chen, Yu-Sheng Chao, Weir-Torn Jiaang

Index: Bioorg. Med. Chem. Lett. 16(12) , 3268-72, (2006)

Full Text: HTML

Abstract

A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats.

Related Compounds

Related Articles:

Evidence for a role of GABA- and glutamate-gated chloride channels in olfactory memory.

2012-11-01

[Pharmacol. Biochem. Behav. 103(1) , 69-75, (2012)]

The effects of local perfusion of DAMGO on extracellular GABA and glutamate concentrations in the rostral ventromedial medulla.

2008-02-01

[J. Neurochem. 104(3) , 806-17, (2008)]

Effects of theanine, r-glutamylethylamide, on neurotransmitter release and its relationship with glutamic acid neurotransmission.

2005-08-01

[Nutr. Neurosci. 8(4) , 219-26, (2005)]

Dissociation between hippocampal neuronal loss, astroglial and microglial reactivity after pharmacologically induced reverse glutamate transport.

2006-12-01

[Neurochem. Int. 49(7) , 691-7, (2006)]

Cerebral neurons of transgenic ALS mice are vulnerable to glutamate release stimulation but not to increased extracellular glutamate due to transport blockade.

2006-06-01

[Exp. Neurol. 199(2) , 281-90, (2006)]

More Articles...